Pembentukan Kokristal Asam Usnat – N-Methyl-DGlucamine dengan Metode Penguapan Pelarut dan Pengaruhnya terhadap Penurunan Interleukin-8 pada Tikus Inflamasi

Fadhila, Muthia and Umar, Salman and Zaini, Erizal (2020) Pembentukan Kokristal Asam Usnat – N-Methyl-DGlucamine dengan Metode Penguapan Pelarut dan Pengaruhnya terhadap Penurunan Interleukin-8 pada Tikus Inflamasi. Jurnal Sains Farmasi & Klinis, 7 (1). pp. 23-30. ISSN 2407-7062

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Abstract

The objective of the research was to prepare the cocrystal of usnic acid -N-methyl-D-glucamine in order to increase solubility, dissolution rate, and decrease IL-8 levels in rats with inflammation. Cocrystal was prepared with a ratio of 1:1 equimolar by a solvent evaporation method using etanol. Characterizations were conducted using Powder X-ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), infrared spectroscopy (FT-IR), and Scanning Electron Microscopy (SEM). The solubility test, dissolution rate test, and determination of interleukin-8 (IL-8) levels in rats were also performed. CO2 free distilled water was used as a media in the solubility test. Meanwhile, CO2 free distilled water with 0.25 % w/v Sodium Lauryl Sulphate (SLS) were used as the media for dissolution rate studies. Both tests were conducted using a UV-Vis spectrophotometer. The determination of IL-8 levels in rat was performed by using an ELISA method. Powder X-ray Diffraction (PXRD) diffractogram showed a new peak compared to diffraction peaks of each component and physical mixture that confirmed the formation of cocrystal, and peak intensity decreased that shown formation of eutectic mixture. The appearance of the DSC thermogram from cocrystal showed different endothermic peaks for both constituent components. The FT-IR spectrum of cocrystal showed a shift of the wave number spectrum compared to pure usnic acid and N-methyl-D-glucamine. Microscopic analysis by SEM showed a change of crystal morphology. The solubility and dissolution rate of cocrystal increased significantly (p<0.05) by 24 and 23 times compared to the pure usnic acid. Cocrystal could reduce IL-8 levels in rats with inflammation equivalent to acetosal (P <0.05). This study concludes, that cocrystal of usnic acid–Nmethyl-D-glucamine can enhance solubility and dissolution rate, and decrease IL-8 levels in rats with inflammation

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